Tenofovir is an epoch-making breakthrough in the treatment of hepatitis B and AIDS

- Dec 22, 2017 -

Tenofovir is an epoch-making breakthrough in the treatment of hepatitis B and AIDS

The successful development of tenofovir and its proven clinical practice have brought new hope to patients with AIDS and hepatitis B, which can be called epoch-making significance.

Tenofovir disoproxil is a novel nucleotide reverse transcriptase inhibitor approved by the U.S. FDA for the treatment of AIDS and hepatitis B (CHB) in October 2001 and 2008, respectively. At present, more than 100 countries, including China, have approved TDF for the treatment of AIDS, and more than 30 countries and territories in the United States have obtained indications of tenofovir for CHB treatment. TDF, an ester precursor to tenofovir, is rapidly hydrolyzed to tenofovir after oral administration and is phosphorylated by cellular kinases to produce tenofovir diphosphate, a pharmacologically active product, Competition with 5'-deoxyadenosine 5'-triphosphate incorporates into the viral DNA chain, blocking replication of the virus due to its lack of 3'-OH groups that lead to prolonged DNA blockage. Tenofovir is the nucleoside (acid) drug which has the strongest anti-HBV activity and the highest resistance barrier so far. Clinical studies have shown that it has good antiviral activity against HBV and HBV with HIV infection. The latest research also shows that tenofovir monotherapy for the treatment of simple HBV infection also has good efficacy and safety. Based on tenofovir's good anti-HBV activity, safety and high genetic barrier, the 2009 AASLD guideline recommends tenofovir as first-line treatment for CHB antiviral therapy.